Drug Information

Drug (ID: DG01633) and It's Reported Resistant Information

• Name: AZD-8835
• Synonyms: AZD8835; AZD-8835; 1620576-64-8; AZD 8835; 1-(4-(5-(5-Amino-6-(5-(tert-butyl)-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1H-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one; UNII-8B97A88D35; 8B97A88D35; 1-(4-{5-[5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl]-1-ethyl-1H-1,2,4-triazol-3-yl}piperidin-1-yl)-3-hydroxypropan-1-one; 1-Propanone, 1-[4-[5-[5-amino-6-[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]-2-pyrazinyl]-1-ethyl-1H-1,2,4-triazol-3-yl]-1-piperidinyl]-3-hydroxy-; 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1H-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one; 1-Propanone, 1-(4-(5-(5-amino-6-(5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl)-2-pyrazinyl)-1-ethyl-1H-1,2,4-triazol-3-yl)-1-piperidinyl)-3-hydroxy-; compound 25 [PMID: 26475521]; GTPL8915; CHEMBL3894518; SCHEMBL15877923; AZD 8835 [WHO-DD]; BDBM185362; BCP20347; EX-A2295; NSC786099; s7966; ZINC145460849; CCG-269444; CS-4984; NSC-786099; NCGC00484075-01; AC-32648; HY-12869; A16352; US9156831, 3; Q27074810; 1-[4-[5-[5-amino-6-[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]-2-; 1-[4-[5-[5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl]-1-ethyl-1,2,4-triazol-3-yl]piperidin-1-yl]-3-hydroxypropan-1-one
• Target: .; NOUNIPROTAC; [1]
• Formula: 7
• IsoSMILES: CCN1C(=NC(=N1)C2CCN(CC2)C(=O)CCO)C3=CN=C(C(=N3)C4=NN=C(O4)C(C)(C)C)N
• InChI: InChI=1S/C22H31N9O3/c1-5-31-19(26-18(29-31)13-6-9-30(10-7-13)15(33)8-11-32)14-12-24-17(23)16(25-14)20-27-28-21(34-20)22(2,3)4/h12-13,32H,5-11H2,1-4H3,(H2,23,24)
• InChIKey: ZGRDYKFVDCFJCZ-UHFFFAOYSA-N
• PubChem CID: 76685059

Type(s) of Resistant Mechanism of This Drug

  UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Breast cancer [ICD-11: 2C60]

Drug Sensitivity Data Categorized by Their Corresponding Mechanisms

Unusual Activation of Pro-survival Pathway (UAPP)

Key Molecule: PI3-kinase alpha (PIK3CA) [1]

• Molecule Alteration: Missense mutation; p.K111N (c.333G>C)
• Sensitive Disease: ER positive breast cancer [ICD-11: 2C60.6]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: PI3K signaling pathway; Inhibition; hsa04151
• In Vivo Model: Female Swiss athymic nude mouse PDX model; Mus musculus

Key Molecule: PI3-kinase alpha (PIK3CA) [1]

• Molecule Alteration: Missense mutation; p.E545K (c.1633G>A)
• Sensitive Disease: ER positive breast cancer [ICD-11: 2C60.6]
• Experimental Note: Revealed Based on the Cell Line Data
• Cell Pathway Regulation: PI3K signaling pathway; Inhibition; hsa04151
• In Vivo Model: Female Swiss athymic nude mouse PDX model; Mus musculus

References

• Ref 1: Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3KAlpha and PI3K Delta, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast CancersMol Cancer Ther. 2016 May;15(5):877-89. doi: 10.1158/1535-7163.MCT-15-0687. Epub 2016 Feb 2.